Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10586956 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
Abstract
A series of 2-(substituted) phenyl and 2-indolyl quinoline derivatives (10a-l) was synthesized by an efficient microwave-assisted, trifluoroacetic acid-catalyzed, solvent-free method. Evaluation of the inhibitory activity led to the identification of two quinoline inhibitors of cholesterol esterase. 2-(1H-Indol-3-yl)-6-nitro-4-phenylquinoline (10l; IC50 = 1.98 μM) was characterized as a mixed-type inhibitor with a pronounced competitive binding mode.
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Authors
Gisela C. Muscia, Stephanie Hautmann, Graciela Y. Buldain, Silvia E. AsÃs, Michael Gütschow,